GPCR19, also known as G protein-coupled bile acid receptor 1 (GPBAR1) or TGR5, is a protein that in humans is encoded by the GPBAR1 gene.TGR5 gene locates on chromosome position 2q35 in humans. Its open reading frame has 993 base pairs, encoding 330 amino acids. High levels of TGR5 mRNA were detected in several organs such as small intestine, stomach, liver, lung, especially placenta and spleen. TGR5 can be activated by bile acids and then it induces cAMP production. As a membrane receptor, TGR5 can be internalized into the cytoplasm in response to its ligands. TGR5 plays important roles in cell signaling pathways such as nuclear factor κB (NF-κB), AKT, and extracellular signalregulated kinases (ERK). Its agonists may be potential drugs for treatment of metabolic, inflammation and digestive disorders. Activation of TGR5 has shown promise in treating various metabolic diseases such as type 2 diabetes (T2D) and obesity. Its activation also mediates novel effects on inflammation and cancer in different organs.


1.Guo C, et al. Front Physiol. 2016;7:646.